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Benzoxaboroles have recently attracted attention in drug discovery as boron-containing skeletons for pharmacologically active compounds with unique mechanisms of action, such as tabborole (a leucyl tRNA synthetase inhibitor) and crisaborole (a PDE4 inhibitor).1,2) Due to the unique property of the boron center forming reversible covalent bonds with diverse nucleophilic functional groups, benzoxaboroles are considered a useful structural element in drug discovery.
We offer a lineup of benzoxaborole derivatives featuring substituents at each substitution position on the benzene ring. These substituents serve as starting points for further functional group transformation reactions, such as condensation reactions and aromatic substitution reactions. Additionally, we can handle custom synthesis and scale-up manufacturing of analogues and derivatives of these compounds.